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Assay Detail

CHEMBL1942167

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of PDK1-mediated AKT1 phosphorylation at T308 in human H460 cells after 2 hrs by ELISA
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type H460
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

3-phosphoinositide-dependent protein kinase 1 (CHEMBL2534)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of novel, potent, and selective inhibitors of 3-phosphoinositide-dependent kinase (PDK1).
Murphy ST, Alton G, Bailey S, Baxi SM, Burke BJ, Chappie TA, Ermolieff J, Ferre R, Greasley S, Hickey M, Humphrey J, Kablaoui N, Kath J, Kazmirski S, Kraus M, Kupchinsky S, Li J, Lingardo L, Marx MA, Richter D, Tanis SP, Tran K, Vernier W, Xie Z, Yin MJ, Yu XH.
J Med Chem (2011) 54 : 8490 -8500
PubMed 22040023 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.74 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1940251 1 6.92
CHEMBL1940252 1 6.80
CHEMBL1940253 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1940251 IC50 = 120.0 nM 6.92
CHEMBL1940252 IC50 = 160.0 nM 6.80
CHEMBL1940253 IC50 = 320.0 nM 6.50